Apelt, Joachim; Ligneau, Xavier; Pertz, Heinz H.; Arrang, Jean-Michel; Ganellin, C. Robin; Schwartz, Jean-Charles; Schunack, Walter; Stark, Holger published the artcile< Development of a New Class of Nonimidazole Histamine H3 Receptor Ligands with Combined Inhibitory Histamine N-Methyltransferase Activity>, COA of Formula: C11H16O2, the main research area is piperidinoalkanamine derivative preparation histamine receptor methyltransferase.
In search of novel ways to enhance histaminergic neurotransmission in the central nervous system, a new class of nonimidazole histamine H3 receptor ligands were developed that simultaneously possess strong inhibitory activity on the main histamine metabolizing enzyme, histamine N-methyltransferase (HMT). The novel compounds contain an aminoquinoline moiety, which is an important structural feature for HMT inhibitory activity, connected by different spacers to a piperidino group (for H3 receptor antagonism). Variation of the spacer structure provides two different series of compounds One series, having only an alkylene spacer between the basic centers, led to highly potent HMT inhibitors with moderate to high affinity at human histamine H3 receptors. The second series possesses a p-phenoxypropyl spacer, which may be extended by another alkylene chain. This latter series also showed strong inhibitory activity on HMT, and in most cases, the H3 receptor affinity even surpassed that of the first series. One of the most potent compounds with this dual mode of action is 4-(4-(3-piperidinopropoxy)phenylamino)quinoline (hH3, Ki = 0.09 nM; HMT, IC50 = 51 nM). This class of compounds showed high antagonist potency and good H3 receptor selectivity in functional assays in guinea pig on H1, H2, and H3 receptors. Because of low or missing in vivo activity of two selected compounds, the proof of concept of these valuable pharmacol. tools for the supposed superior overall enhancing effect on histaminergic neurotransmission failed to appear hitherto.
Journal of Medicinal Chemistry published new progress about Drug screening. 52244-70-9 belongs to class ethers-buliding-blocks, and the molecular formula is C11H16O2, COA of Formula: C11H16O2.
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem